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Drug intelligence / Profile preview
MCT4 antisense oligonucleotide (MCT4 ASO) is a preclinical synthetic antisense oligonucleotide designed to target and downregulate monocarboxylate transporter 4 (MCT4) mRNA expression. MCT4 is a plasma membrane transporter that mediates the efflux of lactic acid and protons, playing a critical role in the reprogrammed glucose metabolism (aerobic glycolysis) of cancer cells. By inhibiting MCT4, the ASO reduces lactic acid secretion, increases intracellular lactate levels, decreases intracellular pH, and suppresses tumor cell proliferation and glycolysis. Developed by the University of British Columbia, Vancouver Prostate Centre, and BC Cancer Agency, and licensed to the spin-off LAST Innovation, MCT4 ASO has demonstrated preclinical efficacy in models of castration-resistant prostate cancer (CRPC), neuroendocrine prostate cancer (NEPC), and bladder cancer. Additionally, research at the University of Guelph has investigated MCT4 antisense oligonucleotides (MCT4 AS-ODN) in the anterior cingulate cortex (ACC) to disrupt astrocyte-neuronal lactate shuttling, showing potential for blocking the development of chronic pain.
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